131I标记新型小分子肽VP2

Preliminary Study of Radioiodination of VP2

  • 摘要: 本文通过双功能偶联剂5-(三正丁基锡)-3-吡啶甲酸-N-琥珀酰亚胺酯(SPC)将131I标记到小分子融合多肽VP2上,研究了131I标记多肽VP2的体内外稳定性及在正常小鼠体内的代谢与分布。结果表明,该标记药物室温下放置48 h后放化纯度仍可达97%,其在小鼠体内可通过胃肠道快速代谢,在甲状腺的摄取较低。用间接标记法得到的131I-SPC-VP2在体内外有良好的稳定性。

     

    Abstract: The VP2 peptide specifically binding to vasoactive intestinal polypeptide receptor 1(VPAC1) receptor was radioiodinated with 131I by bi-functional linker N-succinimidyl 5-(tributylstannyl)-3-pyridinecarboxylate (SPC), and in vitro and in vivo stability of the labeled peptide were evaluated. Mice were injected intravenously with either 1.2×106 Bq 131I-SPC-VP2 or Na 131I. Radiochemical purity and biodistribution were studied at various time points. The result showed that purified 131I-SPC-VP2 exhibited radiochemical purity of 97% at room temperature up to 48 h. The tissue uptake of 131I-SPC-VP2 was low after 6 h injection, especially in thyroid. The result indicated the labeled compound had fast clearance and good stability in vivo.

     

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